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"What, sir, would you make a ship sail against the wind and currents by lighting a bonfire under her deck? I pray you, excuse me, I have not the time to listen to such nonsense."
Napoleon Bonaparte ; When told of the Robert Fulton steamboat
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| Number | Title | Issue Date |
| 7960564 | Crystalline chemotherapeutic N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N′-(2-fluoro-5-methylphenyl)urea Crystalline Form 1, ways to make it, formulations comprising it and made with it and methods of treating patients having disease using it are disclosed. ... | 06/14/2011 |
| 7947843 | Crystalline chemotherapeutic N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N′-(2-fluoro-5-methylphenyl)urea Hydrate Crystalline Form 1, ways to make it, formulations comprising it and made with it and methods of treating patients having disease using it are disclosed. ... | 05/24/2011 |
| 7943782 | Crystalline chemotherapeutic N-(4-(3-Amino-1H-indazol-4-yl)phenyl)-N′-(2-fluoro-5-methylphenyl)urea Tolueneate Crystalline Form 1, ways to make it and ways to use it are disclosed. ... | 05/17/2011 |
| 7799930 | 1-alkyl-3-aminoindazoles Methods of making 1-alkylindazoles are described. The methods involve reacting a 2-alkylaminobenzonitrile with a nitrosating agent followed by reduction-cyclization of the resulting nitrosamine to form a 1-alkyl-3-aminoindazole. The 1-alkyl-3-aminoindazole can be de... | 09/21/2010 |
| 7772404 | Crystalline form 2 of the chemotherapeutic N-[4-(3-amino-1H-indazol-4-yl)phenyl]-N′-(2-fluoro-5-methylphenyl)urea N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N′-(2-fluoro-5-methylphenyl)urea Crystalline Form 2, ways to make it, formulations comprising it and made with it and methods of treating patients having disease using it are disclosed. ... | 08/10/2010 |
| 7390803 | Tetrahydropyranyl cyclopentyl benzylamide modulators of chemokine receptor activity The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28... | 06/24/2008 |
| 7365211 | Heterocyclic GABAA subtype selective receptor modulators This invention relates to a method for modulating α2 subtype GABAA receptors with heterocyclic compounds of formula I, and salts, solvates and prodrugs thereof. The invention further relates to said heterocyclic compounds and pharmaceutical co... | 04/29/2008 |
| 7321045 | Vitronectin receptor antagonist pharmaceuticals The present invention describes novel compounds of the formula: (Q)d-Ln-Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. Th... | 01/22/2008 |
| 7309713 | Use of the non-opiate analgesic drug flupirtine for the treatment of overactive bladder and associated diseases including urge incontinence, urinary flow problems as a result of prostate hyperplasia and irritable bowel syndrome The present invention is directed to the prevention, reversal and medical treatment of lower urinary tract dysfunction including bladder instability and other related diseases as described below including urinary flow problems, urgency and incontinence as a result o... | 12/18/2007 |
| 7297709 | Indazole, benzisoxazole, and benzisothiazole kinase inhibitors Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using th... | 11/20/2007 |
| 7214699 | Indazole derivatives as CRF antagonists This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein R3 is optionally substituted aryl or heteroaryl, R1... | 05/08/2007 |
| 7166629 | Aminoindazole derivatives as medicaments and pharmaceutical compositions including them The present invention relates to novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or h... | 01/23/2007 |
| 7138418 | Pentafluorobenzenesulfonamides and analogs The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states... | 11/21/2006 |
| 7102001 | Process for preparing pyrrolotriazine The present invention provides a process for preparing compounds of formula (I) or a pharmaceutically acceptable salt thereof. The compounds prepared by the process of the invention inhibit tyrosine kinas... | 09/05/2006 |
| 7019011 | Aminoindazole derivatives as medicaments and pharmaceutical compositions including them The present invention relates to novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or heteroar... | 03/28/2006 |
| 7015233 | Fused compounds that inhibit vanilloid subtype 1 (VR1) receptor Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity. ... | 03/21/2006 |
| 7001905 | Substituted diarylamines as MEK inhibitors Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are us... | 02/21/2006 |
| 6949579 | Aminoindazole derivatives and intermediates, preparation thereof, and pharmaceutical compositions thereof The present invention relates to the novel indazole derivatives of general formula (I): in which: R is either O, S or NH; R3 is an alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, aryl, heterocycle, cycloalkyl, alk... | 09/27/2005 |
| 6933390 | Process for the arylation of aza-heterocycles with activated aromatics in presence of caesium carbonate The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of fur... | 08/23/2005 |
| 6914069 | Pharmaceutically active compounds and methods of use The invention provides substituted pyrazole compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility. ... | 07/05/2005 |
| 6906070 | Guanidine mimics as factor Xa inhibitors The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are use... | 06/14/2005 |
| 6858638 | Substituted indazoles, compositions containing them, method of production and use Substituted indazoles, compositions containing them, method of production and use. The present invention relates in particular to novel specific substituted indazoles exhibiting kinase-inhibiting activity, having therapeutic activity, in particlar in oncology. ... | 02/22/2005 |
| 6855722 | Substituted indoles and their use as integrin antagonists The present invention relates to novel substituted indole compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts, and pharmaceutical comp... | 02/15/2005 |
| 6794518 | Vitronectin receptor antagonist pharmaceuticals The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer ... | 09/21/2004 |
| 6762189 | 5-pyrimidinecarboxamide derivatives and the pharmaceutical compositions containing said derivatives The present invention relates to novel 5-pyrimidinecarboxamide derivatives and the pharmaceutical compositions containing said derivatives, and more specifically, to 5-pyrimidinecarboxamide derivatives and their pharmacutically able salts, the process for preparing ... | 07/13/2004 |
| 6716841 | Nitrogen containing heterobicycles as factor Xa inhibitors This invention relates generally to nitrogen containing heterobicycles of formulas A and B: which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the s... | 04/06/2004 |
| 6613743 | Sulfonamide inhibitors of aspartyl protease The present invention relates to a novel class of sulfonamides of formula I which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and phy... | 09/02/2003 |
| 6593349 | Bisarylamines as potassium channel openers Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides bisarylamines, compositions... | 07/15/2003 |
| 6534535 | Inhibitors of factor Xa Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of formula (I) below: ##STR1## are useful in vitro or in vivo for preventing or treating coagulation disorders.... | 03/18/2003 |
| 6358993 | Pharmaceutically active nitrogen ring compounds and methods of use thereof The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-... | 03/19/2002 |
| 6262040 | Indazole derivatives and their use as inhibitors of phosphodiesterase (PDE) type IV and the production of tumor necrosis factor (TNF) The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R, R1, and R2, are as defined herein. The invention further relates to pharmaceutical compositions containing, and methods of us... | 07/17/2001 |
| 6214834 | Integrin inhibitor prodrugs This invention relates to novel heterocycles which are useful as antagonists of the vଲ.sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, to iontophoretic d... | 04/10/2001 |
| 5891881 | Aminoheterocycle-substituted glycerols Aminoheterocycle-substituted glycerols of Formula I are disclosed: ##STR1## wherein one of A, B or C is --X--R, wherein X is --O-- or --S--, and R is a substituted or unsubstituted C12-24 alkyl or alkenyl, the substituent being one or more... | 04/06/1999 |
| 5840738 | Selective ଲ-3 adrenergic agonists The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective 댣 adrenergic receptor agonists useful in the treatment of Type II diabet... | 11/24/1998 |
| 5756532 | Aminomethyl-2 3 8 9-tetrahydro-7H-1 4-dioxino2 3-E!-indol-8-ones and derivatives The compounds of formula I: ##STR1## wherein R1 and R2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R1 and R2, taken together, are benzylidene optionally substituted with R3 as defin... | 05/26/1998 |
| 5750547 | Certain carbanate anti-cancer agents The present invention is concerned with novel anticancer agents having potent antineoplastic activity without systemic toxicity and mutagenicity. The novel anticancer agents of the present invention are derivatives of formula I: ##STR1## wherein... | 05/12/1998 |
| 5714606 | Pyrrolidine-containing monomers and oligomers The invention relates to pyrrolidine monomeric units and to oligomers which are joined via phosphate linkages, including phosphorothioate, phosphodiester and phosphoramidate linkages.... | 02/03/1998 |
| 5631381 | Process for the preparation of pesticidal 1-(haloaryl) heterocyclic compounds Process for preparing complex pesticidal 1-(haloaryl)heterocyclic compounds by reacting 1-(nitroaryl)heterocycles with metallic halide salts.... | 05/20/1997 |
| 5543433 | Azine-substituted phenylacetic acid derivatives and fungicides containing these Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro, Y is an amino, methylamino or dimethylamino group, Z is a group CHCH3, CHOCH3 or NOCH3, R is hydrogen or alk... | 08/06/1996 |
| 5519134 | Pyrrolidine-containing monomers and oligomers Novel pyrrolidine monomers bearing various functional groups are used to prepare oligomeric structures. The pyrrolidine monomers can be joined via standard phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups... | 05/21/1996 |
